Novel FabH Inhibitor, showing potent antibacterial activity with a MIC value of 3.89–7.81 μM−1 against the tested bacterial strains and exhibiting potent E. coli FabH inhibitory activity with an IC 50 value of 1.6 μM

Novel clickable fumarate-competitive chemoproteomic probe

Novel pyrimidine synthesis inhibitor, exhibiting low micromolar antiviral activity against various influenza A and B virus strains, including the highly pathogenic influenza A strains H5N1 and H7N9, enterovirus A71, respiratory syncytial virus, human rhin

Novel matrix metalloproteinase inhibitor, reducing secretion of very low density lipoprotein-triacylglycerol, lowering TAG levels in serum and the liver, VLDL-TAG secretion, de novo FA synthesis in the liver, and serum levels of insulin and glucose

Novel and potent inhibitor of PCAF catalytic domain

Selective, potent inhibitor of the late current mediated by the cardiac isoform of the sodium channel (NaV1.5)

Novel bactericidal, killing Mycobacterium tuberculosis by targeting iron-sulfur protein Rv0338c (IspQ), a putative redox sensor

Novel bactericidal, killing Mycobacterium tuberculosis by targeting iron-sulfur protein Rv0338c (IspQ), a putative redox sensor

Novel potent and selective MAP4K4 inhibitor

Novel antifungal agent against Candida albicans persister cells

Novel influenza A hemagglutinin (HA) fusion inhibitor (EC 50 = 1.9 ± 0.3 μM), preventing HA from transitioning to the postfusion state at pH 5.0

Polyethylene glycol conjugate of SN38, acting as a topoisomerase I inhibitor,, exerting significant anti-leukaemia activity, overcoming ABCG2-mediated topotecan resistance

Novel potent MCT1 inhibitor, exhibiting good single agent anticancer efficacy properties

Novel Dual-Analyte Fluorescent Chemosensor for Visualizing Neurotransmitter Exocytosis

Topoisomerase I inhibitor

Potent and selective SIRT1 inhibitor

Novel glucagon-like peptide 1 (GLP-1) receptor agonist, displaying significantly elongated half-lives and improved long-acting antidiabetic activity in the presence of endogenous anti-DNP antibodies

Novel ALK5 inhibitor

Novel partial positive allosteric GABAA receptor modulator

Novel GluN2B antagonist, binding at the same GluN1/GluN2B dimer interface as ifenprodil but adopting a remarkably different binding mode involving a distinct subcavity and receptor interactions

Novel potent gamma-secretase modulator

The first plant cyclic peptide with antibacterial and antifungal activity

Scavenger for oxidative species such as peroxynitrite, superoxide, and hydrogen peroxide

Novel negative allosteric modulator (NAM) of NMDA receptors, reducing both the overall current that flows following receptor activation and the flux of Ca2+ ion relative to monovalent cations

Novel Biased modulator of NMDA receptors, controlling channel opening and ion selectivity

Novel broad-spectrum β-lactamase inhibitor

Potent and selective inhibitor of Pim 1, inhibiting the phosphorylation of Bad and 4EBP1 in cells and suppresses the proliferation of several non-solid and solid human tumor cell lines.

Pesticide, acting as antibiotics or growth regulators to kill mites and ticks

Partial agonist at the glutamate binding site of the GluN2 subunits

Novel enhancer of the religation reaction of human topoisomerase I